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抗疟新药青蒿素(Artemisinin)的某些含氮衍生物在动物实验中还显示局部麻醉效应。本工作利用分化的NG108-15细胞,在全细胞电压箝位下,比较了五种青篙素衍生物和普鲁卡因对电压门控钢流(INa)和延迟整流钾流(IK)的作用。所观察的五种衍生物均部分可逆地和剂量依赖地抑制INa,其中含芳香环的SM541作用最强,效应与普鲁卡因的相近。300μmol/L普鲁卡因对IK只有微弱的抑制作用;而五种衍生物在相同浓度下均明显抑制IK,并加快它的失活;其中除SM541外,还观察到在药物持续灌流下,对IK幅度的抑制效应迅速降低。
Some of the nitrogen-containing derivatives of the new malaria drug Artemisinin also show a local anesthetic effect in animal experiments. In this work, the differentiated NG108-15 cells were used to compare the effects of five kinds of derivatives of luteolin and procaine on voltage-gated steel currents (INa) and delayed rectifier potassium currents (IK) under the condition of whole cell voltage clamp effect. All of the five derivatives observed inhibited INa partially and reversibly and dose-dependently. The aromatic ring-containing SM541 had the strongest effect and similar effect to procaine. 300μmol / L procaine weakly inhibited IK; while the five derivatives at the same concentration significantly inhibited IK, and accelerate its inactivation; in addition to SM541, it was also observed in the continuous drug infusion, The inhibition of IK amplitude decreases rapidly.